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GPCR/G protein

G protein–coupled receptors (GPCRs) which are also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR), constitute a large protein family of receptors, that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times.

Products for GPCR/G protein

  1. Cat.No. Product Name Information
  2. BCC5709 CCK Octapeptide, non-sulfated CCK Octapeptide, non-sulfated
  3. BCC5971 HU 308 Potent and selective CB2 agonist HU 308
  4. BCC7481 CP 154526 CP 154526
  5. BCC7076 Ghrelin (human) Endogenous ghrelin receptor agonist Ghrelin (human)
  6. BCC5767 Ghrelin (rat) Ghrelin (rat)
  7. BCC5882 BVD 10 Highly selective NPY Y1 receptor antagonist; devoid of Y4 agonist activity BVD 10
  8. BCC6916 (S)-(-)-Pindolol (S)-(-)-Pindolol
  9. BCC7888 EMDT oxalate EMDT oxalate is a selective 5-HT EMDT oxalate
  10. BCC7464 AG 045572 Selective GnRH receptor antagonist AG 045572
  11. BCC7687 S 25585 S 25585
  12. BCC7906 Methyl 5-{2-[(tert-butylamino)carbothioyl]carbohydrazonoyl}-1-(2,4-difluorophenyl)-1H-pyrazole-4-carboxylate GPR35 antagonist Methyl 5-{2-[(tert-butylamino)carbothioyl]carbohydrazonoyl}-1-(2,4-difluorophenyl)-1H-pyrazole-4-carboxylate
  13. BCC7635 SSR 146977 hydrochloride SSR 146977 hydrochloride
  14. BCC7120 MRS 1706 MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS 1706
  15. BCC7473 MRS 1754 MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats. MRS 1754
  16. BCC7838 Zotepine Zotepine
  17. BCC1885 Reparixin Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively. Reparixin
  18. BCC1886 Reparixin L-lysine salt Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. Reparixin L-lysine salt
  19. BCC5739 [Nphe1]Nociceptin(1-13)NH2 [Nphe1]Nociceptin(1-13)NH2
  20. BCC4340 Timolol Maleate (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction. Timolol Maleate
  21. BCC7034 Sphingosine-1-phosphate Endogenous agonist at S1P1-5 Sphingosine-1-phosphate
  22. BCC7660 LY 393558 LY 393558
  23. BCC4975 Ticagrelor Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation. Ticagrelor
  24. BCC6127 MS 245 oxalate MS 245 oxalate
  25. BCC7179 WAY 161503 hydrochloride WAY 161503 hydrochloride
  26. BCC7570 UDP disodium salt Uridine-5'-diphosphate disodium salt is a potent, selective P2Y6 receptor native agonist (EC50=300 nM; pEC50=6.52) and a potent P2Y14 antagonist (pEC50=7.28). Uridine-5'-diphosphate disodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis. UDP disodium salt
  27. BCC5214 Nicergoline Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. Nicergoline
  28. BCC7030 VUF 5574 VUF 5574
  29. BCC6108 8-Aminoadenine Adenine receptor agonist 8-Aminoadenine
  30. BCC7380 JTE 907 JTE 907
  31. BCC4409 NPS-2143 NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. NPS-2143
  32. BCC4410 BML-190 Potent, selective CB2 ligand,BML-190 is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. BML-190
  33. BCC7983 MA 2029 MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility. MA 2029
  34. BCC4972 SB408124 SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. SB408124
  35. BCC1387 Avosentan Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist. Avosentan
  36. BCC5180 Guanfacine Guanfacine is a selective α2A receptor agonist. Guanfacine
  37. BCC1609 Guanfacine hydrochloride Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors. Guanfacine hydrochloride
  38. BCC5754 [Ala11,22,28]VIP [Ala11,22,28]VIP
  39. BCC5947 DOB hydrochloride DOB hydrochloride
  40. BCC7629 NPS ALX Compound 4a dihydrochloride NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist with an IC50 of 7.2 nM, which also has a great binding affinity with Ki of 0.2 nM. NPS ALX Compound 4a dihydrochloride
  41. BCC6683 HEAT hydrochloride HEAT hydrochloride
  42. BCC1910 RS 504393 RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively). RS 504393
  43. BCC6827 Oleamide Oleamide is an endogenous fatty acid amide which can be synthesized de novo in the mammalian nervous system, and has been detected in human plasma. Oleamide
  44. BCC7708 LU AA33810 LU AA33810
  45. BCC4032 AVE 0991 AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM. AVE 0991
  46. BCC4222 AVE 0991 sodium salt AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21±35 nM. AVE 0991 sodium salt
  47. BCC7376 IBC 293 IBC 293
  48. BCC1610 GW-1100 GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9. GW-1100
  49. BCC5953 [Des-octanoyl]-Ghrelin (rat) [Des-octanoyl]-Ghrelin (rat)
  50. BCC7203 Alytesin Alytesin
  51. BCC5029 SKI II SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation. SKI II
  52. BCC7539 THIQ THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants. THIQ
  53. BCC1650 Indacaterol Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist. Indacaterol
  54. BCC6438 Regadenoson Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing. Regadenoson
  55. BCC5708 Bombesin Bombesin is a tetradecapeptide originally isolated from frog skin; plays an important role in the release of gastrin and the activation of G-protein receptors. Bombesin
  56. BCC7304 [Des-octanoyl]-Ghrelin (human) [Des-octanoyl]-Ghrelin (human)
  57. BCC6265 PU 02 PU 02
  58. BCC5750 [cPP1-7,NPY19-23,Ala31,Aib32,Gln34] - hPancreatic Polypeptide [cPP1-7,NPY19-23,Ala31,Aib32,Gln34] - hPancreatic Polypeptide
  59. BCC7372 SCH 442416 SCH 442416
  60. BCC7487 O-1602 O-1602
  61. BCC4336 Propranolol HCl Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used to control hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. Propranolol HCl
  62. BCC7902 [D-Trp8]-γ-MSH [D-Trp8]-γ-MSH
  63. BCC7612 SCH 221510 SCH 221510
  64. BCC1808 NPS-2143 hydrochloride NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. NPS-2143 hydrochloride
  65. BCC5770 tcY-NH2 tcY-NH2
  66. BCC5489 Labetalol HCl Labetalol hydrochloride is a mixed alpha/beta adrenergic antagonist that is used to treat high blood pressure. Labetalol HCl
  67. BCC4318 DL-Adrenaline DL-Epinephrine is the racemate of epinephrine. L-Epinephrine is a hormone secreted by the medulla of the adrenal glands. L-Epinephrine is an α-adrenergic and β-adrenergic receptor agonist. DL-Adrenaline
  68. BCC7878 AS 1269574 GPR119 receptor agonist AS 1269574
  69. BCC6237 LUF 5834 LUF 5834
  70. BCC1332 AH 6809 AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors. AH 6809
  71. BCC1363 Anamorelin Fumarate Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay. Anamorelin Fumarate
  72. BCC5993 Lys-Bradykinin Lys-Bradykinin
  73. BCC5884 Urotensin II-related peptide Urotensin II-related peptide
  74. BCC6364 OXA (17-33) OXA (17-33)
  75. BCC4322 Acebutolol HCl Acebutolol hydrochloride is a β1 adrenergic receptor (β1AR) antagonist. Acebutolol hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. Acebutolol HCl
  76. BCC6257 SB 611812 SB 611812
  77. BCC7405 SUN-B 8155 SUN-B 8155
  78. BCC7853 TCS 2510 TCS 2510
  79. BCC7422 J 113863 J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J 113863
  80. BCC4560 Ki16198 Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6. Ki16198
  81. BCC1155 Ki16425 Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells. Ki16425
  82. BCC6051 Novokinin Novokinin
  83. BCC5804 NECA 5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist. NECA
  84. BCC6024 [Ala17]-MCH [Ala17]-MCH
  85. BCC7474 B-HT 933 dihydrochloride B-HT 933 dihydrochloride
  86. BCC7450 TC 1 TC 1
  87. BCC7954 (±)-SLV 319 (±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM. (±)-SLV 319
  88. BCC7316 Prostaglandin E2 Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation. Prostaglandin E2
  89. BCC4408 Cinacalcet HCl Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment. Cinacalcet HCl
  90. BCC5931 AR-M 1896 GAL2 agonist AR-M 1896
  91. BCC5880 MRS 2279 MRS 2279
  92. BCC7910 TC 14012 TC 14012
  93. BCC6911 Zinterol hydrochloride Zinterol (MJ 9184) is a potent and selective β2-adrenoceptor agonist. Zinterol increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM. Zinterol hydrochloride
  94. BCC7714 SB 612111 hydrochloride SB 612111 hydrochloride
  95. BCC7670 TCS OX2 29 TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1. TCS OX2 29
  96. BCC7161 2-Chloro-N6-cyclopentyladenosine Potent, selective A1 agonist 2-Chloro-N6-cyclopentyladenosine
  97. BCC6859 Zaprinast Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs). Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects. Zaprinast
  98. BCC1868 Preladenant Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors. Preladenant
  99. BCC4765 Betamethasone Betamethasone is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties. Betamethasone
  100. BCC5778 [(pF)Phe4]Nociceptin(1-13)NH2 [(pF)Phe4]Nociceptin(1-13)NH2
  101. BCC6188 YE 120 YE 120

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